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Drug Delivery

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https://www.readbyqxmd.com/read/28645219/pullulan-microbeads-si-hpmc-hydrogel-injectable-system-for-the-sustained-delivery-of-gdf-5-and-tgf-%C3%AE-1-new-insight-into-intervertebral-disc-regenerative-medicine
#1
Nina Henry, Johann Clouet, Audrey Fragale, Louise Griveau, Claire Chédeville, Joëlle Véziers, Pierre Weiss, Jean Le Bideau, Jérôme Guicheux, Catherine Le Visage
Discogenic low back pain is considered a major health concern and no etiological treatments are today available to tackle this disease. To clinically address this issue at early stages, there is a rising interest in the stimulation of local cells by in situ injection of growth factors targeting intervertebral disc (IVD) degenerative process. Despite encouraging safety and tolerability results in clinic, growth factors efficacy may be further improved. To this end, the use of a delivery system allowing a sustained release, while protecting growth factors from degradation appears of particular interest...
November 2017: Drug Delivery
https://www.readbyqxmd.com/read/28644728/liposomes-equipped-with-cell-penetrating-peptide-br2-enhances-chemotherapeutic-effects-of-cantharidin-against-hepatocellular-carcinoma
#2
Xue Zhang, Congcong Lin, Aiping Lu, Ge Lin, Huoji Chen, Qiang Liu, Zhijun Yang, Hongqi Zhang
A main hurdle for the success of tumor-specific liposomes is their inability to penetrate tumors efficiently. In this study, we incorporated a cell-penetrating peptide BR2 onto the surface of a liposome loaded with the anticancer drug cantharidin (CTD) to create a system targeting hepatocellular carcinoma (HCC) cells more efficiently and effectively. The in vitro cytotoxicity assay comparing the loaded liposomes' effects on hepatocellular cancer HepG2 and the control Miha cells showed that CTD-loaded liposomes had a stronger anticancer effect after BR2 modification...
November 2017: Drug Delivery
https://www.readbyqxmd.com/read/28644090/transdermal-administration-of-melatonin-coupled-to-cryopass-laser-treatment-as-noninvasive-therapy-for-prostate-cancer
#3
Laura Terraneo, Paola Bianciardi, Eleonora Virgili, Elena Finati, Michele Samaja, Rita Paroni
Melatonin, a pineal gland hormone, exerts oncostatic activity in several types of human cancer, including prostate, the most common neoplasia and the third most frequent cause of male cancer death in the developed world. The growth of androgen-sensitive LNCaP prostate cancer cells in mice is inhibited by 3 mg/kg/week melatonin (0.09 mg/mouse/week) delivered by i.p. injections, which is equivalent to a dose of 210 mg/week in humans. The aim of this study is to test an alternative noninvasive delivery route based on transdermal administration of melatonin onto the tumor area followed by cryopass-laser treatment...
November 2017: Drug Delivery
https://www.readbyqxmd.com/read/28633548/polyquaternium-mediated-delivery-of-morpholino-oligonucleotides-for-exon-skipping-in-vitro-and-in-mdx-mice
#4
Mingxing Wang, Bo Wu, Sapana N Shah, Peijuan Lu, Qilong Lu
Antisense oligonucleotide therapy for Duchenne muscular dystrophy has shown great potential in preclinical and clinical trials, but its therapeutic applications are still limited due to inefficient delivery. In this study, we investigated a few polyquaterniums (PQs) with different size and composition for their potential to improve delivery performance of an antisense phosphorodiamidate morpholino oligomer (PMO) both in vitro and in vivo. The results showed that Luviquat(TM) series, especially PQ-1 and PQ-3, promoted the exon-skipping efficiency comparable to Endoporter-mediated PMO delivery in vitro...
November 2017: Drug Delivery
https://www.readbyqxmd.com/read/28633547/lipid-based-nanosystem-of-edaravone-development-optimization-characterization-and-in-vitro-in-vivo-evaluation
#5
Ankit Parikh, Krishna Kathawala, Chun Chuan Tan, Sanjay Garg, Xin-Fu Zhou
Edaravone (EDR) is a well-recognized lipophilic free radical scavenger for diseases including neurodegenerative disease, cardiovascular disease, and cancer. However, its oral use is restricted due to poor oral bioavailability (BA). The aim of present research was to enable its oral use by developing a lipid-based nanosystem (LNS). The components of LNS including oil, surfactants, and co-surfactants were selected based on their potential to maximize the solubilization in gastrointestinal (GI) fluids, reduce its glucuronidation and improve transmembrane permeability...
November 2017: Drug Delivery
https://www.readbyqxmd.com/read/28618841/assessment-of-solid-microneedle-rollers-to-enhance-transmembrane-delivery-of-doxycycline-and-inhibition-of-mmp-activity
#6
Abbie Omolu, Maryse Bailly, Richard M Day
Many chronic wounds exhibit high matrix metalloproteinase (MMP) activity that impedes the normal wound healing process. Intradermal delivery (IDD) of sub-antimicrobial concentrations of doxycycline, as an MMP inhibitor, could target early stages of chronic wound development and inhibit further wound progression. To deliver doxycycline intradermally, the skin barrier must be disrupted. Microneedle rollers offer a minimally invasive technique to penetrate the skin by creating multiple microchannels that act as temporary conduits for drugs to diffuse through...
November 2017: Drug Delivery
https://www.readbyqxmd.com/read/28617150/atorvastatin-loaded-nanostructured-lipid-carriers-nlcs-strategy-to-overcome-oral-delivery-drawbacks
#7
Mohammed Elmowafy, Hany M Ibrahim, Mohammed A Ahmed, Khaled Shalaby, Ayman Salama, Hossam Hefesha
Atorvastatin (AT) is a widely used lipid-regulating drug to reduce cholesterol and triglycerides. Its poor aqueous solubility and hepatic metabolism require development of drug delivery systems able to improve its solubility and bypass hepatic effect. For this purpose, atorvastatin nanostructured lipid carriers (AT-NLCs) were prepared and characterized. AT-NLCs were prepared by emulsification using high-speed homogenization followed by ultrasonication. The prepared NLCs showed particle size between 162.5 ± 12 and 865...
November 2017: Drug Delivery
https://www.readbyqxmd.com/read/28597700/engineering-of-a-novel-optimized-platform-for-sublingual-delivery-with-novel-characterization-tools-in-vitro-evaluation-and-in-vivo-pharmacokinetics-study-in-human
#8
Nadia M Morsi, Ghada A Abdelbary, Ahmed H Elshafeey, M Abdallah Ahmed
The aim of this work was to develop a novel and more efficient platform for sublingual drug delivery using mosapride citrate (MSP) as a model drug. The engineering of this delivery system had two stages, the first stage was tuning of MSP physicochemical properties by complexation with pure phosphatidylcholine or phosphatidylinositol enriched soybean lecithin to form MSP-phospholipid complex (MSP-PLCP). Changes in physicochemical properties were assessed and the optimum MSP-PLCP formula was then used for formulation into a flushing resistant platform using two mucoadhesive polymers; sodium alginates and sodium carboxymethylcellulose at different concentrations...
November 2017: Drug Delivery
https://www.readbyqxmd.com/read/28585867/characterization-of-transgene-expression-and-pdna-distribution-of-the-suctioned-kidney-in-mice
#9
Natsuko Oyama, Yuki Fuchigami, Shintaro Fumoto, Megumu Sato, Masayori Hagimori, Kazunori Shimizu, Shigeru Kawakami
We have previously developed an efficient and safe transfection method for the kidney in mice: renal suction-mediated transfection. In this study, we verified the detailed characteristics of transgene expression and plasmid DNA (pDNA) in mice to develop therapeutic strategies and application to gene function analysis in the kidney. After naked pDNA was administered intravenously, the right kidney was immediately suctioned by a tissue suction device. We examined the spatial distribution of transgene expression and pDNA in the suctioned kidney using tissue clearing by CUBIC, Clear(T2), and Scale SQ reagents...
November 2017: Drug Delivery
https://www.readbyqxmd.com/read/28574335/toxicity-of-orally-inhaled-drug-formulations-at-the-alveolar-barrier-parameters-for-initial-biological-screening
#10
Eleonore Fröhlich
Oral delivery is the most common mode of systemic drug application. Inhalation is mainly used for local therapy of lung diseases but may also be a promising route for systemic delivery of drugs that have poor oral bioavailability. The thin alveolar barrier enables fast and efficient uptake of many molecules and could deliver small molecules and proteins, which are susceptible to degradation and show poor absorption by oral application. The low rate of biotransformation and proteolytic degradation increases bioavailability of drugs but accumulation of not absorbed material may impair normal lung function...
November 2017: Drug Delivery
https://www.readbyqxmd.com/read/28574300/anti-cd123-antibody-modified-niosomes-for-targeted-delivery-of-daunorubicin-against-acute-myeloid-leukemia
#11
Fu-Rong Liu, Hui Jin, Yin Wang, Chen Chen, Ming Li, Sheng-Jun Mao, Qiantao Wang, Hui Li
A novel niosomal delivery system was designed and investigated for the targeted delivery of daunorubicin (DNR) against acute myeloid leukemia (AML). Anti-CD123 antibodies conjugated to Mal-PEG2000-DSPE were incorporated into normal niosomes (NS) via a post insertion method to afford antibody-modified niosomes (CD123-NS). Next, NS was modified with varying densities of antibody (0.5 or 2%, antibody/Span 80, molar ratio), thus providing L-CD123-NS and H-CD123-NS. We studied the effect of antibody density on the uptake efficiency of niosomes in NB4 and THP-1 cells, on which CD123 express differently...
November 2017: Drug Delivery
https://www.readbyqxmd.com/read/28574291/temperature-sensitive-heparin-modified-poloxamer-hydrogel-with-affinity-to-kgf-facilitate-the-morphologic-and-functional-recovery-of-the-injured-rat-uterus
#12
He-Lin Xu, Jie Xu, Si-Si Zhang, Qun-Yan Zhu, Bing-Hui Jin, De-Li ZhuGe, Bi-Xin Shen, Xue-Qing Wu, Jian Xiao, Ying-Zheng Zhao
Endometrial injury usually results in intrauterine adhesion (IUA), which is an important cause of infertility and recurrent miscarriage in reproductive women. There is still lack of an effective therapeutic strategy to prevent occurrence of IUA. Keratinocyte growth factor (KGF) is a potent repair factor for epithelial tissues. Here, a temperature-sensitive heparin-modified poloxamer (HP) hydrogel with affinity to KGF (KGF-HP) was used as a support matrix to prevent IUA and deliver KGF. The rheology of KGF-HP hydrogel was carefully characterized...
November 2017: Drug Delivery
https://www.readbyqxmd.com/read/28549383/reversed-lipid-based-nanoparticles-dispersed-in-oil-for-malignant-tumor-treatment-via-intratumoral-injection
#13
Liao Shen, Zhen Zhang, Tao Wang, Xi Yang, Ri Huang, Dongqin Quan
Intratumoral injection of anticancer drugs directly delivers chemotherapeutics to the tumor region, offering an alternative strategy for cancer treatment. However, most hydrophilic drugs spread quickly from the injection site into systemic circulation, leading to inferior antitumor activity and adverse effects in patients. Therefore, we developed novel reversed lipid-based nanoparticles (RLBN) as a nanoscale drug carrier. RLBNs differ from traditional nanoscale drug carriers in that they possess a reversed structure consisting of a polar core and lipophilic periphery, leading to excellent solubility and stability in hydrophobic liquids; therefore, hydrophilic drugs can be entrapped in RLBNs and dispersed in oil...
November 2017: Drug Delivery
https://www.readbyqxmd.com/read/28535740/etodolac-transdermal-cubosomes-for-the-treatment-of-rheumatoid-arthritis-ex-vivo-permeation-and-in-vivo-pharmacokinetic-studies
#14
Salwa Salah, Azza A Mahmoud, Amany O Kamel
In this study, transdermal etodolac-loaded cubosomes were developed in order to relieve patient pain and joints stiffness by providing stable etodolac concentration at the targeting sites through controlled drug delivery via the noninvasive skin route with more sustaining and less frequent dosing. Different ratios and percentages of poloxamer 407 and monoolein were used to formulate the cubosomes using emulsification and homogenization processes. The etodolac-loaded cubosomes showed particle size values ranging from 135...
November 2017: Drug Delivery
https://www.readbyqxmd.com/read/28532223/preliminary-study-on-fabrication-characterization-and-synergistic-anti-lung-cancer-effects-of-self-assembled-micelles-of-covalently-conjugated-celastrol-polyethylene-glycol-ginsenoside-rh2
#15
Peng Li, XiaoYue Zhou, Ding Qu, Mengfei Guo, Chenyi Fan, Tong Zhou, Yang Ling
The aim of this study was to develop an amphipathic polyethylene glycol (PEG) derivative that was bi-terminally modified with celastrol and ginsenoside Rh2 (Celastrol-PEG-G Rh2). Such derivative was capable of forming novel, celastrol-loaded polymeric micelles (CG-M) for endo/lysosomal delivery and thereby synergistic treatment of lung cancer. Celastrol-PEG-G Rh2 with a yield of 55.6% was first synthesized and characterized. Its critical micellar concentration was 1 × 10(-5 )M, determined by pyrene entrapment method...
November 2017: Drug Delivery
https://www.readbyqxmd.com/read/28509629/nanoparticle-based-delivery-enhances-anti-inflammatory-effect-of-low-molecular-weight-heparin-in-experimental-ulcerative-colitis
#16
Tawfek Yazeji, Brice Moulari, Arnaud Beduneau, Valentin Stein, Dirk Dietrich, Yann Pellequer, Alf Lamprecht
Epithelial administration of low molecular weight heparin (LMWH) has proven its therapeutic efficiency in ulcerative colitis (UC) but still lacks of a sufficiently selective drug delivery system. Polymeric nanoparticles were used here not only to protect LMWH from intestinal degradation but also to provide targeted delivery to inflamed tissue in experimental colitis mice. LMWH was associated with polymethacrylate nanoparticles (NP) type A (PEMT-A) or type B (PEMT-B) of a size: 150 nm resulting in a maximum drug loading: 0...
November 2017: Drug Delivery
https://www.readbyqxmd.com/read/28509588/peg-lipid-plga-hybrid-nanoparticles-loaded-with-berberine-phospholipid-complex-to-facilitate-the-oral-delivery-efficiency
#17
Fei Yu, Mingtao Ao, Xiao Zheng, Nini Li, Junjie Xia, Yang Li, Donghui Li, Zhenqing Hou, Zhongquan Qi, Xiao Dong Chen
The natural product berberine (BBR), present in various plants, arouses great interests because of its numerous pharmacological effects. However, the further development and application of BBR had been hampered by its poor oral bioavailability. In this work, we report on polymer-lipid hybrid nanoparticles (PEG-lipid-PLGA NPs) loaded with BBR phospholipid complex using a solvent evaporation method for enhancing the oral BBR efficiency. The advantage of this new drug delivery system is that the BBR-soybean phosphatidylcholine complex (BBR-SPC) could be used to enhance the liposolubility of BBR and improve the affinity with the biodegradable polymer to increase the drug-loading capacity and controlled/sustained release...
November 2017: Drug Delivery
https://www.readbyqxmd.com/read/28509581/dexamethasone-distribution-characteristic-following-controllable-continuous-sub-tenon-drug-delivery-in-rabbit
#18
Xuetao Huang, Manqiang Peng, Yezhen Yang, Yiqin Duan, Kuanshu Li, Shaogang Liu, Changhua Ye, Ding Lin
Drug delivery systems are required to be safe, minimally invasive and effectively delivery drug to the target tissues. But delivery drugs to the eye has not yet satisfied this need. Here, we focused on examining the distribution of dexamethasone (DEX) in ocular and plasmic samples following controllable continuous sub-Tenon drug delivery (CCSDD) of dexamethasone disodium phosphate (DEXP) in rabbit, and to compare that with two traditional routes: subconjunctival injection and intravenous injection. The DEX concentration was analyzed by Shimadzu LC-MS 2010 system...
November 2017: Drug Delivery
https://www.readbyqxmd.com/read/28502199/ceramide-lipid-based-nanosuspension-for-enhanced-delivery-of-docetaxel-with-synergistic-antitumor-efficiency
#19
Tianqi Wang, Lixia Feng, Shaomei Yang, Yongjun Liu, Na Zhang
Ceramide (CE), a bioactive lipid with tumor suppression, has been widely used as a drug carrier and enhancer for cancer therapy. CE-based combination therapy was prone to be attractive in cancer therapy. In our previous study, the combination of CE and docetaxel (DTX) was proved to be an effective strategy for cancer therapy. To further improve the antitumor efficiency of DTX, the CE lipid-based nanosuspensions (LNS) was prepared for the delivery of DTX to exhibit synergistic therapeutic effect. The enhanced delivery and synergistic therapeutic effect of DTX-loaded CE-LNS (CE + DTX-LNS) were evaluated...
November 2017: Drug Delivery
https://www.readbyqxmd.com/read/28480758/loratadine-bioavailability-via-buccal-transferosomal-gel-formulation-statistical-optimization-in-vitro-in-vivo-characterization-and-pharmacokinetics-in-human-volunteers
#20
Mohammed H Elkomy, Shahira F El Menshawe, Heba A Abou-Taleb, Marwa H Elkarmalawy
Loratadine (LTD) is an antihistaminic drug that suffers limited solubility, poor oral bioavailability (owing to extensive first-pass metabolism), and highly variable oral absorption. This study was undertaken to develop and statistically optimize transfersomal gel for transbuccal delivery of LTD. Transfersomes bearing LTD were prepared by conventional thin film hydration method and optimized using sequential Quality-by-Design approach that involved Placket-Burman design for screening followed by constrained simplex-centroid design for optimization of a Tween-80/Span-60/Span-80 mixture...
November 2017: Drug Delivery
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